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19

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T62061	COX-2-IN-6	COX; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	COX-2-IN-6 是一种具有有效性、选择性且可口服的环氧化酶-2 (COX-2) 抑制剂，对 COX-2 具有抑制作用，IC50 为 0.84 μM，Ki 为 69 nM。COX-2-IN-6 对 COX-2 驱动的 PGE2 合成具有抑制作用，IC50 为 0.60 μM。COX-2-IN-6 可用于预防结直肠癌。
T28958	TG6-129 TG6 129	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	TG6-129 是有效的EP2受体选择性拮抗剂，可降低 butaprost 诱导的 P388D1 巨噬细胞中炎症因子的表达。
T63943	COX-2-IN-10
	COX-2-IN-10 是 COX-2 的有效抑制剂。COX-2-IN-10 对 IL-6、TNF-α 和 IL-1β 的产生表现出抑制作用。COX-2-IN-10 能够浓度依赖性地抑制 PGE2 的产生，其 IC50 值为 2.54 μM。COX-2-IN-10 在 mRNA 和蛋白水平上抑制 iNOS 和 COX-2 的表达。
T79362	COX-2/15-LOX-IN-4	Lipoxygenase	Metabolism
	COX-2/15-LOX-IN-4（compound 5i）是一种针对COX-2和15-LOX的双重抑制剂，其IC50值分别为0.075 μM和1.97 μM。该化合物能有效地阻止LPS诱发的细胞内促炎细胞因子（IL-6, ROS）的产生，表现出明确的抗炎活性。
T79361	COX-2/15-LOX-IN-3	Lipoxygenase	Metabolism
	COX-2/15-LOX-IN-3 (compound 5k) 为COX-2/15-LOX的一种双重抑制剂，具有分别为0.075 μM和1.97 μM的IC50值。该化合物能显著抑制LPS诱导的细胞产生促炎细胞因子（IL-6, ROS和NO），表明其具备显著的抗炎活性。
T60433	NF-κB-IN-6
	NF-κB-IN-6 (Compound 3d) 是通过抑制NF-κB 信号通路减少 iNOS 和 COX-2 蛋白的表达的抗炎剂。NF-κB-IN-6 抑制脂多糖诱导的 RAW264.7 细胞中 NO 的生成，IC50值为 23.1 μM。
T11995	Melatonin-d4 N-Acetyl-5-methoxytryptamine D5,Melatonin D5,褪黑素 D5	Others	Others
	Melatonin D5, a deuterium-labeled version of melatonin, is a hormone produced by the pineal gland, known for its role as a selective ATF-6 inhibitor that promotes apoptosis in human hepatoma cells via COX-2 downregulation. Additionally, it activates melatonin receptors and exhibits antioxidative and anti-inflammatory properties.
T68919	Nabumetone Alcohol
	Nabumetone alcohol is the alcohol form of nabumetone, a non-steroidal anti-inflammatory drug (NSAID) that is rapidly metabolized in the liver to a major active metabolite, 6-methoxy-2-naphthyl acetic acid, which inhibits the cyclooxygenase enzyme and preferentially blocks COX-2 activity (which is indirectly responsible for the production of inflammation and pain during arthritis).
T36070	(±)5(6)-EET
	5(6)-EET is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5(6)-EET degrades into 5,6-DiHET and 5(6)-δ-lactone, which can be converted to 5(6)-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5(6)-EET has been implicated in the mobilization of calcium and hormone secretion. 5(6)-EET is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhib...
T71212	Lornoxicam-d4
	Lornoxicam-d4 is intended for use as an internal standard for the quantification of lornoxicam by GC- or LC-MS. Lornoxicam is a COX inhibitor and non-steroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic properties. It inhibits production of thromboxane B2 from arachidonic acid in HEL human erythroleukemic cells, which endogenously express COX-1, as well as inhibits LPS-induced formation of prostaglandin F1α from arachidonic acid in Mono-Mac-6 cells, which endogenously e...
T71285	Metaxalone-d6
	Metaxalone-d6 is intended for use as an internal standard for the quantification of metaxalone by GC-or LC-MS. Metaxalone is a skeletal muscle relaxant. It inhibits the proliferation of, and induces apoptosis in, RAW 264.7 cells in vitro when used at concentrations ranging from 1 to 100 µM. Metaxalone also reduces LPS-induced increases in COX-1, COX-2, and NF-kB levels and inhibits LPS-induced production of TNF-α, IL-6, and prostaglandin E2 in RAW 264.7 cells. Formulations containing metaxalone ...
T71303	Flufenamic Acid-d4
	Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear...
T83773	Prostaglandin E2 Inhibitor 3 PGE2 Inhibitor 3
	Prostaglandin E2抑制剂3是一种microsomal prostaglandin E合酶-1 (mPGES-1; IC50 = 0.2 µM)的抑制剂，相较于COX-1、COX-2、5-lipoxygenase (5-LO)和soluble epoxide hydrolase (sEH)，在10 µM的无细胞试验中表现出对mPGES-1的选择性。在10 µM和1 µM的浓度下，该抑制剂能抑制A549细胞中IL-1β诱导的PGE2生成以及在J774A.1巨噬细胞中，LPS诱导的IL-6和PGE2生成。同时，它还能抑制由钙离子载体A23187单独或结合花生四烯酸和A23187诱导的5-LO产物形成，包括白三烯B4 (LTB4) 和5-H(p)ETE（IC50s分别为4.9和5.2 µM）。在体内，10 mg/kg剂量的Prostaglandin E2抑制剂3能防止在zymosan诱导的小鼠腹膜炎模型中白细胞渗入腹腔液中。
T36152	14S(15R)-EET
	14S(15R)-EET is an oxylipin and a cytochrome P450 metabolite of arachidonic acid .114S(15R)-EET binds to isolated guinea pig monocytes with a Kivalue of 612.5 nM in a competitive binding assay using [3H]14(15)-EET.2It induces dilation of precontracted isolated canine epicardial arterioles (EC50= 4 pM) and denuded porcine subepicardial arterioles (EC50= 3 pM).3Unlike 14R(15S)-EET, 14S(15R)-EET does not inhibit COX in enzyme assays or isolated platelets.4 1.Daikh, B.E., Lasker, J.M., Raucy, J.L., ...
T35789	Palmitic acid-1-13C
	Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6 \|1. Santos, M.J., López-Jurado, M., Llopis, J., et a...
T35881	Resolvin E2
	Resolvin E2 (RvE2) is a member of the specialized pro-resolving mediator (SPM) family of bioactive lipids.1It is produced from eicosapentaenoic acidviaan 18-HEPE intermediate, which is formed by aspirin-acetylated COX-2-mediated oxidation of EPA, by 5-lipoxygenase (5-LO) in human polymorphonuclear (PMN) neutrophils.2,3RvE2 (20 ng/animal) inhibits increases in inflammatory exudate neutrophil infiltration in a mouse model of peritonitis induced by zymosan A .3Hepatic RvE2 levels are increased in m...
T35791	Palmitic acid-13C
	Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid-13C contains 13C at the C2 position and has been used in the study of free fatty acid incorporation into phospholipid fatty acids in soil microbes.1 Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.2 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.3 Palmitic ...
T36176	AMK (hydrochloride)
	AMK is an active metabolite of the neurohormone melatonin .1,2,3,4It is formed from melatoninviathe metabolic intermediate AFMK that is then deformylated by catalase or formamidase.5,6AMK scavenges singlet oxygenin vitrowhen used at a concentration of 200 μM.1It inhibits the epinephrine- and arachidonic acid-induced production of prostaglandin E2and PGD2in ovine seminal vesicle microsomes in a concentration- and time-dependent manner, as well as LPS-induced increases in COX-2 levels in RAW 264.7...
T35597	Neuromedin U-23 (rat) (trifluoroacetate salt)
	Neuromedin U-23 (NMU-23) is a neuropeptide involved in diverse biological processes, including smooth muscle contraction, energy homeostasis, and nociception.1It is an agonist of neuromedin-U receptor 1 (NMUR1; EC50= 0.17 nM for the human receptor in a calcium mobilization assay using HEK293 cells) and NMUR2 (EC50= ~1.4-2 nM for arachidonic acid release in CHO cells expressing the human receptor).2,3NMU-23 (1 μM) induces contractions in isolated rat colon smooth muscle strips.4It decreases body ...

化合物

Cat.No: T62061

Target: COX, Prostaglandin Receptor

Cat.No: T28958

Synonym: TG6 129

Target: Prostaglandin Receptor

Cat.No: T63943

COX-2/15-LOX-IN-4

Cat.No: T79362

Target: Lipoxygenase

COX-2/15-LOX-IN-3

Cat.No: T79361

Target: Lipoxygenase

Cat.No: T60433

Cat.No: T11995

Synonym: N-Acetyl-5-methoxytryptamine D5,Melatonin D5,褪黑素 D5

Target: Others

Nabumetone Alcohol

Cat.No: T68919

Cat.No: T36070

Cat.No: T71212

Cat.No: T71285

Flufenamic Acid-d4

Cat.No: T71303

Prostaglandin E2 Inhibitor 3

Cat.No: T83773

Synonym: PGE2 Inhibitor 3

Cat.No: T36152

Palmitic acid-1-13C

Cat.No: T35789

Cat.No: T35881

Palmitic acid-13C

Cat.No: T35791

AMK (hydrochloride)

Cat.No: T36176

Neuromedin U-23 (rat) (trifluoroacetate salt)

Cat.No: T35597

Cat. No.	Product Name	Target	Signaling Pathways
TN1308	6-Hydroxyflavanone	Others; Lipoxygenase; COX; GABA Receptor	Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; Others
	6-Hydroxyflavanone 是从菖蒲叶中提取分离，通过靶向环氧合酶-2（COX-2），5-脂氧合酶（5-LOX）以及阿片类药物和 GABA-A 受体从而具有抗炎和抗神经性疼痛活性。6-Hydroxyflavanone 在链脲佐菌素诱导的糖尿病神经病变模型中具有抗伤害感受特性。
T7113	Paradol 姜酮酚,6-paradol,必理通,[6]-Gingerone	COX	Immunology/Inflammation; Neuroscience
	Paradol ([6]-Gingerone) 是一种姜科植物中发现的酚类天然产物，具有抗癌、抗炎、抗氧化和神经保护作用。在小鼠皮肤癌变中，可结合到环氧合酶(COX-2) 活性位点。
T6S1917	Schisandrol B Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B	P450; Reactive Oxygen Species; Autophagy	Autophagy; Immunology/Inflammation; Metabolism; NF-κB
	Schisandrol B (Besigomsin) 是华中五味子的主要活性成分，具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生，也抑制 P-糖蛋白和CYP3A 的活性。
T7030	anemarsaponin B 知母皂苷B,知母皂苷 B	p38 MAPK; NF-κB; MEK; COX; NO Synthase	Immunology/Inflammation; MAPK; Neuroscience; NF-κB
	Anemarsaponin B 是一种甾体皂苷，可降低iNOS 和COX-2的蛋白和 mRNA 水平，减少促炎细胞因子的表达和产生。它通过阻断 IκBα 的磷酸化来抑制NF-κB 的 p65 亚基的核转位，还抑制 MAP 激酶激酶 3/6 (MKK3/6) 和混合谱系激酶 3 的磷酸化。
T6S1684	8-Gingerol	Antioxidant; Antibacterial; TRP/TRPV Channel	Membrane transporter/Ion channel; Microbiology/Virology; oxidation-reduction
	8-Gingerol 分离自姜的根状茎，是口服有效的 TRPV1激活剂，EC50值为5.0 µM。8-Gingerol 抑制 COX-2，还能抑制体外 H. pylori 的生长。
T35741	Gliovirin
	Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decrease...

天然产物

6-Hydroxyflavanone

Cat.No: TN1308

Target: Others, Lipoxygenase, COX, GABA Receptor

Cat.No: T7113

Synonym: 姜酮酚,6-paradol,必理通,[6]-Gingerone

Target: COX

Cat.No: T6S1917

Synonym: Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B

Target: P450, Reactive Oxygen Species, Autophagy

anemarsaponin B

Cat.No: T7030

Synonym: 知母皂苷B,知母皂苷 B

Target: p38 MAPK, NF-κB, MEK, COX, NO Synthase

Cat.No: T6S1684

Target: Antioxidant, Antibacterial, TRP/TRPV Channel

Cat.No: T35741

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